Topoisomerase I Inhibitors

Compounds that inhibit the activity of DNA TOPOISOMERASE I.
DrugDrug NameDrug Indication
DB00762IrinotecanFor the treatment of metastatic colorectal cancer (first-line therapy when administered with 5-fluorouracil and leucovorin). Also used in combination with cisplatin for the treatment of extensive small cell lung cancer. Irinotecan is currently under investigation for the treatment of metastatic or recurrent cervical cancer. Also used in combination with fluorouracil and leucovorin for the treatment of patients with metastatic adenocarcinoma of the pancreas after disease progression following gemcitabine-based therapy.
DB01030TopotecanFor the treatment of advanced ovarian cancer in patients with disease that has recurred or progressed following therapy with platinum-based regimens. Also used as a second-line therapy for treatment-sensitive small cell lung cancer, as well as in combination with cisplatin for the treatment of stage IV-B, recurrent, or persistent cervical cancer not amenable to curative treatment with surgery and/or radiation therapy.
DB04690CamptothecinInvestigated for the treatment of cancer.
DB06159RubitecanInvestigated for use/treatment in pancreatic cancer, leukemia (unspecified), melanoma, ovarian cancer, and cancer/tumors (unspecified).
DB12185ExatecanNot Available
DB12459BelotecanNot Available
DB054827-ethyl-10-hydroxycamptothecinInvestigated for use/treatment in colorectal cancer.
DB14951Etirinotecan pegolNot Available
DrugDrug NameTargetType
DB00762IrinotecanDNA topoisomerase I, mitochondrialtarget
DB00762IrinotecanDNA topoisomerase 1target
DB00762IrinotecanCytochrome P450 3A4enzyme
DB00762IrinotecanCytochrome P450 3A5enzyme
DB00762IrinotecanUDP-glucuronosyltransferase 1-1enzyme
DB00762IrinotecanUDP-glucuronosyltransferase 1-9enzyme
DB00762IrinotecanLiver carboxylesterase 1enzyme
DB00762IrinotecanCytochrome P450 3A7enzyme
DB00762IrinotecanCytochrome P450 2B6enzyme
DB00762IrinotecanSolute carrier family 22 member 3transporter
DB00762IrinotecanSolute carrier organic anion transporter family member 1B1transporter
DB00762IrinotecanMultidrug resistance-associated protein 1transporter
DB00762IrinotecanATP-binding cassette sub-family G member 2transporter
DB00762IrinotecanSerum albumincarrier
DB00762IrinotecanCocaine esteraseenzyme
DB00762IrinotecanMultidrug resistance protein 1transporter
DB00762IrinotecanCanalicular multispecific organic anion transporter 1transporter
DB01030TopotecanDNA topoisomerase I, mitochondrialtarget
DB01030TopotecanDNA topoisomerase 1target
DB01030TopotecanATP-binding cassette sub-family G member 2transporter
DB01030TopotecanMultidrug resistance protein 1transporter
DB01030TopotecanCytochrome P450 3A4enzyme
DB01030TopotecanMultidrug and toxin extrusion protein 1transporter
DB01030TopotecanMultidrug and toxin extrusion protein 2transporter
DB04690CamptothecinDNA topoisomerase 1target
DB04690CamptothecinMultidrug resistance protein 1transporter
DB04690CamptothecinATP-binding cassette sub-family G member 2transporter
DB04690CamptothecinSerum albumincarrier
DB06159RubitecanDNA topoisomerase 1target
DB054827-ethyl-10-hydroxycamptothecinDNA topoisomerase 1target
DB054827-ethyl-10-hydroxycamptothecinCytochrome P450 3A4enzyme